Corticotropin-releasing factor peptide antagonists: design, characterization and potential clinical relevance.

Abstract:

:Elusive for more than half a century, corticotropin-releasing factor (CRF) was finally isolated and characterized in 1981 from ovine hypothalami and shortly thereafter, from rat brains. Thirty years later, much has been learned about the function and localization of CRF and related family members (Urocortins 1, 2 and 3) and their 2 receptors, CRF receptor type 1 (CRFR1) and CRF receptor type 2 (CRFR2). Here, we report the stepwise development of peptide CRF agonists and antagonists, which led to the CRFR1 agonist Stressin1; the long-acting antagonists Astressin2-B which is specific for CRFR2; and Astressin B, which binds to both CRFR1 and CRFR2.This analog has potential for the treatment of CRF-dependent diseases in the periphery, such as irritable bowel syndrome.

journal_name

Front Neuroendocrinol

authors

Rivier JE,Rivier CL

doi

10.1016/j.yfrne.2013.10.006

subject

Has Abstract

pub_date

2014-04-01 00:00:00

pages

161-70

issue

2

eissn

0091-3022

issn

1095-6808

pii

S0091-3022(13)00069-1

journal_volume

35

pub_type

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